Abstract
Though all the marketed drugs of dipeptidyl peptidase IV inhibitors are structurally different, their inherent correlation is worthy of further investigation. Herein we rapidly discovered a novel DPP-IV inhibitor 8g (IC50 = 4.9 nmol.L-1) which exhibits as good activity and selectivity as the market drugs through scaffold hopping and drug splicing strategies based on alogliptin and linagliptin. This study demonstrated that the employment of classic medicinal chemistry strategy to the marketed drugs with specific target is an efficient approach to discover novel bioactive molecules.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Dipeptidyl-Peptidase IV Inhibitors / chemical synthesis*
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Dipeptidyl-Peptidase IV Inhibitors / chemistry
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Drug Design*
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Drug Discovery / methods*
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Humans
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Hypoglycemic Agents / chemical synthesis*
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Hypoglycemic Agents / chemistry
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Linagliptin / chemical synthesis
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Linagliptin / chemistry
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Molecular Structure
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Piperidines / chemical synthesis
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Piperidines / chemistry
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Structure-Activity Relationship
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Uracil / analogs & derivatives
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Uracil / chemical synthesis
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Uracil / chemistry
Substances
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Dipeptidyl-Peptidase IV Inhibitors
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Hypoglycemic Agents
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Piperidines
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Linagliptin
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Uracil
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alogliptin